It is estimated that more than 2-3 million people die of malaria each year, and many more suffer from debilitating infection. Approximately a third of the world's population lives in malaria-endemic areas, including Central and South America, Asia, and Africa. Transient visitors or workers in these areas also are at ever-increasing risk of contracting malaria. Mosquitoes that carry malaria parasites have become resistant to insecticides, and the deadliest parasites have become resistant to previously effective antimalarial drugs such as chloroquine and other clinically used agents. New effective antimalarial chemotherapy agents are urgently needed. The present invention provides useful new antimalarial compounds and pharmaceutical compositions, as well as methods of using such antimalarial compounds and pharmaceutical compositions to prevent or treat malaria. These and other objects and advantages of the present invention, as well as additional inventive features, will be apparent from the description of the invention provided herein.